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Page 1
Discovery and Optimization of a Novel Triazole Series of GPR142 Agonists for the Treatment of Type 2 Diabetes.
Guo L, Parker DL, Zang Y, Sweis RF, Liu W, Sherer EC, Buist N, Terebetski J, Kelly T, Bugianesi R, Priest BT, Dingley KH, Li X, Mitelman S, Salituro G, Trujillo ME, Pachanski M, Kirkland M, Powles MA, Eiermann GJ, Feng Y, Shang J, Howard AD, Ujjainwalla F, Sinz CJ, Debenham JS, Edmondson SD, Nargund RP, Hagmann WK, Li D. Guo L, et al. Among authors: powles ma. ACS Med Chem Lett. 2016 Oct 12;7(12):1107-1111. doi: 10.1021/acsmedchemlett.6b00314. eCollection 2016 Dec 8. ACS Med Chem Lett. 2016. PMID: 27994747 Free PMC article.
Discovery of Chromane Propionic Acid Analogues as Selective Agonists of GPR120 with in Vivo Activity in Rodents.
Adams GL, Velazquez F, Jayne C, Shah U, Miao S, Ashley ER, Madeira M, Akiyama TE, Di Salvo J, Suzuki T, Wang N, Truong Q, Gilbert E, Zhou D, Verras A, Kirkland M, Pachanski M, Powles M, Yin W, Ujjainwalla F, Venkatraman S, Edmondson SD. Adams GL, et al. ACS Med Chem Lett. 2016 Dec 6;8(1):96-101. doi: 10.1021/acsmedchemlett.6b00394. eCollection 2017 Jan 12. ACS Med Chem Lett. 2016. PMID: 28105282 Free PMC article.
Design, Synthesis, and Evaluation of Novel and Selective G-protein Coupled Receptor 120 (GPR120) Spirocyclic Agonists.
Cox JM, Chu HD, Chelliah MV, Debenham JS, Eagen K, Lan P, Lombardo M, London C, Plotkin MA, Shah U, Sun Z, Vaccaro HM, Venkatraman S, Suzuki T, Wang N, Ashley ER, Crespo A, Madeira M, Leung DH, Alleyne C, Ogawa AM, Souza S, Thomas-Fowlkes B, Di Salvo J, Weinglass A, Kirkland M, Pachanski M, Powles MA, Tozzo E, Akiyama TE, Ujjainwalla F, Tata JR, Sinz CJ. Cox JM, et al. Among authors: powles ma. ACS Med Chem Lett. 2016 Nov 17;8(1):49-54. doi: 10.1021/acsmedchemlett.6b00360. eCollection 2017 Jan 12. ACS Med Chem Lett. 2016. PMID: 28105274 Free PMC article.
Discovery of benzofuran propanoic acid GPR120 agonists: From uHTS hit to mechanism-based pharmacodynamic effects.
Lombardo M, Bender K, London C, Plotkin MA, Kirkland M, Mane J, Pachanski M, Geissler W, Cummings J, Habulihaz B, Akiyama TE, Di Salvo J, Madeira M, Pols J, Powles MA, Finley MF, Johnson E, Roussel T, Uebele VN, Crespo A, Leung D, Alleyne C, Trusca D, Lei Y, Howard AD, Ujjainwalla F, Tata JR, Sinz CJ. Lombardo M, et al. Among authors: powles ma. Bioorg Med Chem Lett. 2016 Dec 1;26(23):5724-5728. doi: 10.1016/j.bmcl.2016.10.054. Epub 2016 Oct 24. Bioorg Med Chem Lett. 2016. PMID: 27815121
Corrigendum to "Discovery of benzofuran propanoic acid GPR120 agonists: From uHTS hit to mechanism-based pharmacodynamic effects" [Bioorg. Med. Chem. Lett. 26 (2016) 5724-5728].
Lombardo M, Bender K, London C, Plotkin MA, Kirkland M, Mane J, Pachanski M, Geissler W, Cummings J, Habulihaz B, Akiyama TE, Di Salvo J, Madeira M, Pols J, Powles MA, Finley MF, Johnson E, Roussel T, Uebele VN, Crespo A, Leung D, Alleyne C, Trusca D, Lei Y, Howard AD, Ujjainwalla F, Tata JR, Sinz CJ. Lombardo M, et al. Among authors: powles ma. Bioorg Med Chem Lett. 2017 Mar 1;27(5):1333. doi: 10.1016/j.bmcl.2017.01.082. Epub 2017 Feb 4. Bioorg Med Chem Lett. 2017. PMID: 28169160 No abstract available.
Discovery of Novel Tricyclic Heterocycles as Potent and Selective DPP-4 Inhibitors for the Treatment of Type 2 Diabetes.
Wu WL, Hao J, Domalski M, Burnett DA, Pissarnitski D, Zhao Z, Stamford A, Scapin G, Gao YD, Soriano A, Kelly TM, Yao Z, Powles MA, Chen S, Mei H, Hwa J. Wu WL, et al. Among authors: powles ma. ACS Med Chem Lett. 2016 Mar 12;7(5):498-501. doi: 10.1021/acsmedchemlett.6b00027. eCollection 2016 May 12. ACS Med Chem Lett. 2016. PMID: 27190600 Free PMC article.
Antidiabetic and antisteatotic effects of the selective fatty acid synthase (FAS) inhibitor platensimycin in mouse models of diabetes.
Wu M, Singh SB, Wang J, Chung CC, Salituro G, Karanam BV, Lee SH, Powles M, Ellsworth KP, Lassman ME, Miller C, Myers RW, Tota MR, Zhang BB, Li C. Wu M, et al. Proc Natl Acad Sci U S A. 2011 Mar 29;108(13):5378-83. doi: 10.1073/pnas.1002588108. Epub 2011 Mar 9. Proc Natl Acad Sci U S A. 2011. PMID: 21389266 Free PMC article.
Ibrexafungerp: An orally active β-1,3-glucan synthesis inhibitor.
Apgar JM, Wilkening RR, Parker DL Jr, Meng D, Wildonger KJ, Sperbeck D, Greenlee ML, Balkovec JM, Flattery AM, Abruzzo GK, Galgoci AM, Giacobbe RA, Gill CJ, Hsu MJ, Liberator P, Misura AS, Motyl M, Nielsen Kahn J, Powles M, Racine F, Dragovic J, Fan W, Kirwan R, Lee S, Liu H, Mamai A, Nelson K, Peel M. Apgar JM, et al. Bioorg Med Chem Lett. 2021 Jan 15;32:127661. doi: 10.1016/j.bmcl.2020.127661. Epub 2020 Nov 4. Bioorg Med Chem Lett. 2021. PMID: 33160023
MK-5204: An orally active β-1,3-glucan synthesis inhibitor.
Apgar JM, Wilkening RR, Parker DL Jr, Meng D, Wildonger KJ, Sperbeck D, Greenlee ML, Balkovec JM, Flattery AM, Abruzzo GK, Galgoci AM, Giacobbe RA, Gill CJ, Hsu MJ, Liberator P, Misura AS, Motyl M, Kahn JN, Powles M, Racine F, Dragovic J, Fan W, Kirwan R, Lee S, Liu H, Mamai A, Nelson K, Peel M. Apgar JM, et al. Bioorg Med Chem Lett. 2020 Sep 1;30(17):127357. doi: 10.1016/j.bmcl.2020.127357. Epub 2020 Jun 19. Bioorg Med Chem Lett. 2020. PMID: 32738971
31 results